Data/hora: 09/06/2024 11:26:12

Provedor de dados: 	Brazilian Journal of Pharmaceutical Sciences	
País: 	Brazil	
Título: 	Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate	
Autores: 	Eloy,Josimar Oliveira; Saraiva,Juliana; Albuquerque,Sérgio de; Marchetti,Juliana Maldonado.	
Data: 	2015-03-01	
Ano: 	2015	
Palavras-chave: 	Ursolic acid; Chaga's Disease; Solid dispersions; Poloxamer 407; Sodium caprate.	
Resumo: 	Ursolic acid is a promising candidate for treatment of Chagas disease; however it has low aqueous solubility and intestinal absorption, which are both limiting factors for bioavailability. Among the strategies to enhance the solubility and dissolution of lipophilic drugs, solid dispersions are growing in popularity. In this study, we employed a mixture of the surfactants poloxamer 407 with sodium caprate to produce a solid dispersion containing ursolic acid aimed at enhancing both drug dissolution and in vivo trypanocidal activity. Compared to the physical mixture, the solid dispersion presented higher bulk density and smaller particle size. Fourier Transform Infrared Spectroscopy results showed hydrogen bonding intermolecular interactions between drug and poloxamer 407. X-ray diffractometry experiments revealed the conversion of the drug from its crystalline form to a more soluble amorphous structure. Consequently, the solubility of ursolic acid in the solid dispersion was increased and the drug dissolved in a fast and complete manner. Taken together with the oral absorption-enhancing property of sodium caprate, these results explained the increase of the in vivo trypanocidal activity of ursolic acid in solid dispersion, which also proved to be safe by cytotoxicity evaluation using the LLC-MK2 cell line.	
Tipo: 	Info:eu-repo/semantics/article	
Idioma: 	Inglês	
Identificador: 	http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000100101	
Editor: 	Universidade de São Paulo, Faculdade de Ciências Farmacêuticas	
Relação: 	10.1590/S1984-82502015000100011	
Formato: 	text/html	
Fonte: 	Brazilian Journal of Pharmaceutical Sciences  v.51 n.1 2015	
Fonte: 	info:eu-repo/semantics/openAccess